A micelle-based stage-by-stage impelled system for efficient doxorubicin delivery  

作　　者：Sunfan Li Fangzhou Li Dong Wan Zuqin Chen Jie Pan Xing-Jie Liang 

机构地区：[1]School of Chemical Engineering and Technology,Tiangong University,Tianjin,300387,PR China [2]CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety,CAS Center for Excellence in Nanoscience,National Center for Nanoscience and Technology of China,No.11,First North Road,Zhongguancun,Beijing,100190,PR China [3]University of Chinese Academy of Sciences,Beijing,100049,PR China [4]Medical School of Chinese PLA,No.28 Fuxing Road,Beijing,100853,PR China [5]Department of Radiology,The First Medical Centre,Chinese PLA General Hospital,Beijing,PR China [6]Department of Radiology,Chinese PAP Guangxi Corps Hospital,Nanning,Guangxi,PR China

出　　处：《Bioactive Materials》2023年第7期783-795,共13页生物活性材料（英文）

基　　金：This work was supported by the National Key Research and Development Program of China(grant Nos.2021YFA1201000 and 2018YFE0117800);the National Natural Science Foundation of China(NSFC)key project(grant No.32030060);the NSFC International Collaboration Key Project(grant No.51861135103);the National Natural Science Foundation of China(grant No.22078246,22178270 and 82102204);The authors also appreciate the support by“the Beijing-Tianjin-Hebei Basic Research Cooperation Project”(19JCZDJC64100);the China Postdoctoral Science Foundation funded project(grant No.2020M680478).

摘　　要：Chemotherapy remains the mainstay of cancer treatment,benefiting millions of patients each year,but the side effects of chemotherapy drugs severely limit their clinical use.Doxorubicin(DOX)can cause various side effects such as heart damage and treatment-related tumors.The effective use of active and passive targeting will improve the clinical application of DOX.Here,TPGS3350 and bioactive peptides were utilized to construct a micelle-based stage-by-stage impelled efficient system(missiles)for DOX delivery(DOX missiles).By taking advantage of the EPR effect,DOX missiles are efficiently enriched at the tumor site.After being cleaved by matrix metalloproteinase2(MMP2),the peptide(VRGD)targets tumor cells to facilitate uptake of the missiles by the tumor cells via receptor-mediated endocytosis.The intracellular activated caspase-3-catalyzed explosion of DOX missiles further enables efficient tumor killing.This study provides an efficient approach for DOX delivery and toxicity reduction.

关 键 词：DOXORUBICIN Delivery PEPTIDE Missiles CHEMOTHERAPY 

分 类 号：R73[医药卫生—肿瘤]